JP2016540048A - 抗菌物質として使用されるロイコトリエンレセプターアンタゴニストおよびそれらの誘導体 - Google Patents
抗菌物質として使用されるロイコトリエンレセプターアンタゴニストおよびそれらの誘導体 Download PDFInfo
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- JP2016540048A JP2016540048A JP2016555929A JP2016555929A JP2016540048A JP 2016540048 A JP2016540048 A JP 2016540048A JP 2016555929 A JP2016555929 A JP 2016555929A JP 2016555929 A JP2016555929 A JP 2016555929A JP 2016540048 A JP2016540048 A JP 2016540048A
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Abstract
Description
R′は、Hあるいは任意に置換されたC1−4アルキルまたは、−NRIIIRIVである;
ここで、RIIIとRIVは独立してH、任意に置換されたC1−4アルキルであるか、あるいは一緒になって複素環を形成する;
R′′は、H、任意に置換されたC1−6アルキルあるいは任意に置換されたC3−6シクロアルキルまたはヘテロシクロアルキルである;
R2はH、または任意に置換されたアルキル、シクロアルキル、ヘテロシクロアルキル、アリールまたはヘテロアリールである;
R3はH、あるいは任意に置換されたC1−4アルキルである;
R4はH、あるいは任意に置換されたC1−4アルキルである;
また上記化合物の薬学的に受容可能な塩類、エステル、アミドあるいはそのプロドラッグも含まれる。
R′はHあるいは任意に置換されたC1−4アルキルまたはNRIIIRIVである、
ここで、RIIIとRIVは独立してH、任意に置換されたC1−4アルキルであるか、あるいは一緒になって複素環を形成する;
R′′は、H、任意に置換されたC1−6アルキルあるいは任意に置換されたC3−6シクロアルキルまたはヘテロシクロアルキルである。
好ましくは、R1は、H、C(O)MeおよびC(O)OR′′から成るグループから選ばれ、R′′はH、あるいはOHで任意に置換されたシクロアルキル(好ましくはC5)である。
R4はH、あるいは任意に置換されたC1−4アルキルである。好ましくは、R4は任意に−OHで置換されたC1−4アルキルである。より好ましくは、R4はH、MeおよびCH2OHから成るグループから選ばれる。
R3はH、あるいは任意に置換されたC1−4アルキルである;
R4はH、あるいは任意に置換されたC1−4アルキルである;
R5はH、あるいは任意に置換されたC1−4アルキルである;
また、R6はH、C1−4アルキル、ヘテロシクロアルキルまたはOR′′′であり、R′′′はH、C1−6アルキル、あるいは任意に置換されたC3−6シクロアルキルである;また上記化合物の薬学的に受容可能な塩類、エステル、アミドあるいはそのプロドラッグも含まれる。
好ましくは、R6はOR′′′である。ここでR′′′はOHで任意に置換されたC3−6シクロアルキルである。
R4はH、MeおよびCH2OHから成るグループから選ばれる;
R5はHまたはMeである。また、R6はOR′′′である。ここでR′′′はOHで任意に置換されたC3−6シクロアルキルである。
R3はH、あるいは任意に置換されたC1−4アルキルである;
R4はH、あるいは任意に置換されたC1−4アルキルである;
R5は、H、あるいは任意に置換されたC1−4アルキルである;
また上記化合物の薬学的に受容可能な塩類、エステル、アミドあるいはそのプロドラッグも含まれる。
好ましくは、アルキルアリール基は−CH2Phまたは−CH2CH2Phである。
組成物はタブレット(たとえばフィルムコーチング錠)であることができる。
使用される化合物が経口投与用組成物として調剤される発明の実施態様では、それらは存続放出配合物あるいは制御放出配合物として調剤されてもよい。
ザフィルルカスト(シグマ アルドリッチ、英国)は16mMの濃度へジメチルスルホキシド中で再懸濁された。最小阻止濃度(MIC)は、0〜4mMのザフィルルカストを含む様々なバクテリアのブロス溶液を使用して導かれた。供試生物の105 cfu/mLが各チューブに加えられ、37℃で1晩インキュベーションされた。MICは可視で成長が観察されなかった濃度として得られた。さらに、ゾーン抑制研究が標準技法を使用して行なわれた。結果は図1に示される。
黄色ブドウ球菌:
ザフィルルカスト=0.03mM
シプロフロキサシン=0.003mM
セフトリアキソン=0.002mM
ザフィルルカスト=0.006mM
セフトリアキソン=>0.029mMシプロフロキサシン=>0.012mM、
ザフィルルカスト=0.006mM
シプロフロキサシン=平均の0.04mM
セフトリアキソン=0.022mM
ザフィルルカストの殺菌力
細菌培養の105 cfu/mLが、ザフィルルカストの様々な濃度で、37℃で3時間インキュベーションされた。このインキュベーションの終わりに、生存数算定が行われた。また生存パーセンテージ(薬剤のない対照と比較して)として結果が記録された。
結果は図2に示される。
Claims (36)
- ミコバクテリウムまたはコリネバクテリウム感染でないグラム陽性菌感染の治療で使用するためのロイコトリエンレセプターアンタゴニスト、またはそれの薬学的に受容可能な塩またはエステル。
- ロイコトリエンレセプターアンタゴニストは、ザフィルルカスト、プランルカスト、MK−886およびジレウトン、それらの誘導体およびプロドラッグから成る群から選択される、請求項1記載のロイコトリエンレセプターアンタゴニスト。
- ミコバクテリウムまたはコリネバクテリウム感染でないグラム陽性菌感染の治療のための、以下の化学式Iを有する化合物;
式中、R1は、H、任意に置換されたC1−4アルキル、C(O)R′あるいはC(O)OR′′である;
R′は、H、あるいは任意に置換されたC1−4アルキルまたは、−NRIIIRIVである;
ここで、RIIIとRIVは独立してH、任意に置換されたC1−4アルキル、あるいは一緒になって複素環を形成する;
R′′は、H、任意に置換されたC1−6アルキルあるいは任意に置換されたC3−6シクロアルキルまたはヘテロシクロアルキルである;
R2はH、または任意に置換されたアルキル、シクロアルキル、ヘテロシクロアルキル、アリールまたはヘテロアリールである;
R3はH、あるいは任意に置換されたC1−4アルキルである;
R4はH、あるいは任意に置換されたC1−4アルキルである;
または前記化合物の薬学的に受容可能な塩、エステル、アミドあるいはそのプロドラッグ。 - R1はH、C(O)Me、およびC(O)OR′′から成る群から選択され、R′′はH、あるいはOHで任意に置換されたシクロアルキルであり、R2はCH3で任意に置換されたアリールである、請求項3記載の化合物。
- R1はH、C(O)Me、およびC(O)OR′′から成る群から選択され、R′′はH、あるいはOHで任意に置換されたシクロアルキル(好ましくはC5)であり、R2はCH3で任意に置換されたアリールであり、R3はHとMeから成る群から選択され、R4はH、MeおよびCH2OHから成る群から選択される、請求項3記載の化合物。
- R3はHおよびMeから成る群から選択され、R4はH、MeおよびCH2OHから成る群から選択され、R5はHまたはMeであり、R6はOR′′′であり、R′′′はOHで任意に置換されたC3−6シクロアルキルである、請求項6記載の化合物。
- R3はHとMeから成る群から選択され、R4はH、MeおよびCH2Oから成る群から選択され、R5はHとMeから成る群から選択される、請求項8記載の化合物。
- 化合物はザフィルルカストまたはそのプロドラッグ、代謝物質あるいは誘導体である、請求項1または3記載の化合物。
- ザフィルルカストの代謝物質または誘導体は、N−[4−(5−アミノ−1−メチル−1H−インドール−3−イルメチル)−3−メトキシベンゾイル]−2−メチル−ベンゼンスルホンアミド、N−[3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)ベンジル]−1H−インドール−5−イル]アセトアミド、N−[1−ヒドロキシメチル−3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)−ベンジル]−1H−インドール−5−イル]アセトアミド、N−[3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)ベンジル]−1−メチル−1H−インドール−5−イル]アセトアミド、[3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)ベンジル]−lH−インドール−5−イル]カルバミン酸シクロペンチルエステル、[3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)ベンジル]−1−メチル−lH−インドール−5−イル]カルバミン酸ヒドロキシシクロペンチルエステル、[1−ヒドロキシメチル−3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)−ベンジル]−1H−インドール−5−イル]カルバミン酸シクロペンチル基エステルおよび[3−[2−メトキシ−4−(トルエン−2−スルホニルアミノカルボニル)ベンジル]−1H−インドール−5−イル]カルバミン酸ヒドロキシシクロペンチルエステルである、請求項10記載の化合物。
- 細菌感染は日和見感染または院内細菌感染である、請求項1から11のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- 細菌感染は、Lsr2をコード化しないバクテリアの種あるいはその同族体による感染である、請求項1から12のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- 感染はブドウ球菌、腸球菌、かん菌、連鎖球菌、およびクロストリジウムから成る群から選択される菌の感染である、請求項1から13のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- 感染は、黄色ブドウ球菌、メチシリン耐性黄色ブドウ球菌、エンテロコッカス−フェカーリス、枯草菌、肺炎連鎖球菌およびクロストリジウム・ディフィシレから成る群から選択される菌の感染である、請求項1から14のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- ロイコトリエンレセプターアンタゴニストまたは化合物が、経口、全身適用、あるいは吸入による、請求項1から15のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- ロイコトリエンレセプターアンタゴニストまたは化合物は、他の薬学的に有効な作用薬と同時か、別個か、連続して投与される、請求項1から16のいずれか1項記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- 薬学的に有効な作用薬は抗菌物質、抗炎症薬あるいは喘息治療に使用される作用薬である、請求項17記載のロイコトリエンレセプターアンタゴニストまたは化合物。
- 細菌感染はミコバクテリウムまたはコリネバクテリウム感染でないグラム陽性菌感染の治療で使用するための、ロイコトリエン・アンタゴニストおよび1つ以上の薬学的に受容可能な添加剤を含む医薬品組成物。
- 細菌感染はミコバクテリウムまたはコリネバクテリウム感染でないグラム陽性菌感染の治療で使用するための、式IからIIIのいずれかの構造を有する化合物と、1つ以上の薬学的に受容可能な添加剤を含む医薬品組成物。
- 細菌感染は日和見感染か院内細菌感染である、請求項19あるいは20記載の医薬品組成物。
- 細菌感染は、Lsr2をコード化しないバクテリアの種あるいはその同族体による感染である、請求項19から21のいずれか1項記載の医薬品組成物。
- 感染はブドウ球菌、腸球菌、かん菌、連鎖球菌、およびクロストリジウムから成る群から選択される菌の感染である、請求項19から22のいずれか1項記載の医薬品組成物。
- 感染は、黄色ブドウ球菌、メチシリン耐性黄色ブドウ球菌、エンテロコッカス−フェカーリス、枯草菌、肺炎連鎖球菌およびクロストリジウム・ディフィシレから成る群から選択される菌の感染である、請求項19から23のいずれか1項記載の医薬品組成物。
- 医薬品組成物が経口、全身適用、あるいは吸入により投与される、請求項19から24のいずれか1項記載の医薬品組成物。
- 医薬品組成物は、他の薬学的に有効な作用薬と同時か、別個か、連続して投与される、請求項19から25のいずれか1項記載の医薬品組成物。
- 薬学的に有効な作用薬は抗菌物質、抗炎症薬あるいは喘息治療に使用される作用薬である、請求項26記載の医薬品組成物。
- 患者の細菌感染を治療する方法であって、
ロイコトリエンレセプターアンタゴニスト、あるいは式IからIIIのいずれかの構造を有する化合物、または請求項19もしくは20記載の医薬品組成物を、必要とする患者に投与することを含み、細菌感染はミコバクテリウムまたはコリネバクテリウム感染ではない方法。 - ロイコトリエンレセプターアンタゴニストは、ザフィルルカスト、プランルカスト、MK−886およびジレウトン、およびそれらの誘導体から成る群から選択される、請求項28記載の方法。
- 細菌感染は日和見感染か院内細菌感染である、請求項28または29記載の方法。
- 細菌感染は、Lsr2をコード化しないバクテリアの種あるいはその同族体による感染である、請求項28から30のいずれか1項記載の方法。
- 感染はブドウ球菌、腸球菌、かん菌、連鎖球菌、およびクロストリジウムから成る群から選択される菌の感染である、請求項28から31のいずれか1項記載の方法。
- 感染は、黄色ブドウ球菌、メチシリン耐性黄色ブドウ球菌、エンテロコッカス−フェカーリス、枯草菌、肺炎連鎖球菌およびクロストリジウム・ディフィシレから成る群から選択される菌の感染である、請求項28から32のいずれか1項記載の方法。
- ロイコトリエンレセプターアンタゴニスト、化合物あるいは医薬品組成物は経口、全身適用、あるいは吸入により投与される、請求項28から33のいずれか1項記載の方法。
- 付加的な薬学的に有効な作用薬が、ロイコトリエンレセプターアンタゴニスト、化合物あるいは医薬品組成物と、同時に、別々にあるいは連続して投与される、請求項28から34のいずれか1項記載の方法。
- 付加的な薬学的に有効な作用薬は抗菌物質、抗炎症薬あるいは喘息治療に使用される作用薬である、請求項35記載の方法。
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